Development of BromoTag: a “bump-and-hole”–PROTAC system to induce potent, rapid, and selective degradation of tagged target proteins
Small-molecule-induced protein depletion technologies, also called inducible degrons,
allow degradation of genetically engineered target proteins within cells and animals. Here …
allow degradation of genetically engineered target proteins within cells and animals. Here …
Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader
Inducing post-translational protein knockdown is an important approach to probe biology
and validate drug targets. An efficient strategy to achieve this involves expression of a …
and validate drug targets. An efficient strategy to achieve this involves expression of a …
The dTAG system for immediate and target-specific protein degradation
Dissection of complex biological systems requires target-specific control of the function or
abundance of proteins. Genetic perturbations are limited by off-target effects …
abundance of proteins. Genetic perturbations are limited by off-target effects …
Structure-guided design of a “bump-and-hole” bromodomain-based degradation tag
Chemical biology tools to modulate protein levels in cells are critical to decipher complex
biology. Targeted protein degradation offers the potential for rapid and dose-dependent …
biology. Targeted protein degradation offers the potential for rapid and dose-dependent …
[HTML][HTML] Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules
Chemical biology strategies for directly perturbing protein homeostasis including the
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …
Targeted protein degradation phenotypic studies using HaloTag CRISPR/Cas9 endogenous tagging coupled with HaloPROTAC3
To assess the role of a protein, protein loss phenotypic studies can be used, most commonly
through mutagenesis RNAi or CRISPR knockout. Such studies have been critical for the …
through mutagenesis RNAi or CRISPR knockout. Such studies have been critical for the …
Continuous evolution of compact protein degradation tags regulated by selective molecular glues
JAM Mercer, SJ DeCarlo, SS Roy Burman, V Sreekanth… - Science, 2024 - science.org
Conditional protein degradation tags (degrons) are usually> 100 amino acids long or are
triggered by small molecules with substantial off-target effects, thwarting their use as specific …
triggered by small molecules with substantial off-target effects, thwarting their use as specific …
HiBiT-SpyTag: A Minimal Tag for Covalent Protein Capture and Degrader Development
The ability to rapidly and selectively modulate cellular protein levels using small molecules
is essential for studying complex biological systems. Degradation tags, such as dTAG, allow …
is essential for studying complex biological systems. Degradation tags, such as dTAG, allow …
Ligand-induced genetic degradation as a tool for target validation
A Yesbolatova, Y Tominari, MT Kanemaki - Drug Discovery Today …, 2019 - Elsevier
Targeted protein degraders, known as proteolysis targeting chimeras (PROTACs), are
drawing more attention as next-generation drugs to target currently undruggable proteins …
drawing more attention as next-generation drugs to target currently undruggable proteins …
[PDF][PDF] Inducible degradation of target proteins through a tractable affinity-directed protein missile system
LM Simpson, TJ Macartney, A Nardin, LJ Fulcher… - Cell Chemical …, 2020 - cell.com
The affinity-directed protein missile (AdPROM) system utilizes specific polypeptide binders
of intracellular proteins of interest (POIs) conjugated to an E3 ubiquitin ligase moiety to …
of intracellular proteins of interest (POIs) conjugated to an E3 ubiquitin ligase moiety to …